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来自猪蛔虫的γ-氨基丁酸(GABA)和乙酰胆碱受体的药理学特性

Pharmacological profiles of the GABA and acetylcholine receptors from the nematode, Ascaris suum.

作者信息

Walker R J, Colquhoun L, Holden-Dye L

机构信息

Department of Physiology and Pharmacology, University of Southampton, U.K.

出版信息

Acta Biol Hung. 1992;43(1-4):59-68.

PMID:1338558
Abstract

The pharmacological profiles of the acetylcholine and GABA receptors of Ascaris muscle have been investigated. Acetylcholine excites the muscle through activation of a nicotinic receptor which resembles the mammalian ganglionic receptor. DMPP is a potent agonist and alpha-bungarotoxin is a weak antagonist. GABA inhibits the muscle through activation of a chloride-linked receptor which in terms of agonist profile resembles the mammalian GABA-A receptor. However, bicuculline is inactive and picrotoxin is a very weak antagonist. Avermectin acts as a non-competitive antagonist at this GABA receptor with an IC-50 value in the low microM range.

摘要

对蛔虫肌肉中乙酰胆碱和GABA受体的药理学特性进行了研究。乙酰胆碱通过激活一种类似于哺乳动物神经节受体的烟碱样受体来兴奋肌肉。二甲基苯基哌嗪(DMPP)是一种强效激动剂,而α-银环蛇毒素是一种弱拮抗剂。GABA通过激活一种与氯离子相关的受体来抑制肌肉,就激动剂特性而言,该受体类似于哺乳动物的GABA-A受体。然而,荷包牡丹碱无活性,印防己毒素是一种非常弱的拮抗剂。阿维菌素在该GABA受体上作为非竞争性拮抗剂起作用,其IC50值在低微摩尔范围内。

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